Applications
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Compared with DMOG (IC50 = 0.75 mM), ML324 potently reduced IE gene expression, with an IC50 value of 10 μM. Besides, ML324 did not affect the expression of the cellular controls Sp1, S15 and TBP. In HFF cells infected with HSV-1, ML324 lowered viral yields in a dose-dependent manner (~ 4 ~ 5 logs at 25 μM) while 1.5 mM of DMOG was required to cause the same reduction.
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Applications
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In a mouse ganglia explant model of latently infected mice, ML324 significantly inhibited viral activity. At the concentration of 50 μM, ML324 reduced the viral yield by 4.5 logs for each ganglia. Immunofluorescent staining of explanted ganglia sections showed that ML324 inhibited viral reactivation events. However, the withdrawal of ML324 resulted in marked viral replication.
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References:
[1]. Rai G, Kawamura A, Tumber A, Liang Y, Vogel JL, Arbuckle JH, Rose NR, Dexheimer TS, Foley TL, King ON, Quinn A, Mott BT, Schofield CJ, Oppermann U,Jadhav A, Simeonov A, Kristie TM, Maloney DJ. Discovery of ML324, a JMJD2 demethylase inhibitor with demonstrated antiviral activity. 2012 Dec 17 [updated 2013 Sep 16]. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
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